Aliskiren hemifumarate

The first in a class, potent and highly selective, direct renin inhibitor with IC50 of 0.6 nM; no significant inhibition on Cathepsin D, Cathepsin E, Pepsin and HIV-1 peptidase (> 50 uM) ; orally bioactive.Hypertension Approved (In Vitro) :Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively.Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration.Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity. (In Vivo) :Aliskiren hemifumarate (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets.Aliskiren hemifumarate (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting.Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia.

173334-58-2

CGP 60536 | CGP60536B | SPP 100

Pharmacology & Drug Discovery

>98% (HPLC)

10 mM in DMSO

CC (C) [C@@H] (CC1=CC (=C (C=C1) OC) OCCCOC) C[C@@H] ([C@H] (C[C@@H] (C (C) C) C (=O) NCC (C) (C) C (=O) N) O) N.CC (C) [C@@H] (CC1=CC (=C (C=C1) OC) OCCCOC) C[C@@H] ([C@H] (C[C@@H] (C (C) C) C (=O) NCC (C) (C) C (=O) N) O) N.C (=C/C (=O) O) \C (=O) O

C64H110N6O16

1219.589

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.